Assay Detail
Functional
CHEMBL769665
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antimalarial activity against Plasmodium falciparum TM4/8.2 wtDHFR
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL1939) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum K1 |
Publication
Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.61 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22901 | — | — | 1 | 7.16 |
| CHEMBL22139 | — | — | 1 | 6.82 |
| CHEMBL22811 | — | — | 1 | 6.51 |
| CHEMBL416373 | — | — | 1 | 6.48 |
| CHEMBL21395 | — | — | 1 | 6.33 |
| CHEMBL416376 | — | — | 1 | 6.17 |
| CHEMBL419055 | — | — | 1 | 5.62 |
| CHEMBL22138 | — | — | 1 | 5.51 |
| CHEMBL22137 | — | — | 1 | 5.45 |
| CHEMBL279948 | — | — | 1 | 5.35 |
| CHEMBL22146 | — | — | 1 | 5.33 |
| CHEMBL118602 | — | — | 1 | 5.30 |
| CHEMBL120123 | — | — | 1 | 5.17 |
| CHEMBL274031 | — | — | 1 | 4.82 |
| CHEMBL56146 | — | — | 1 | 4.82 |
| CHEMBL291931 | — | — | 1 | 4.76 |
| CHEMBL119224 | — | — | 1 | 4.72 |
| CHEMBL325533 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22901 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL22139 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL22811 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL416373 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL21395 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL416376 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL419055 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL22138 | — | IC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL22137 | — | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL279948 | — | IC50 | = | 4480.0 | nM | 5.35 |
| CHEMBL22146 | — | IC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL118602 | — | IC50 | = | 5060.0 | nM | 5.30 |
| CHEMBL120123 | — | IC50 | = | 6840.0 | nM | 5.17 |
| CHEMBL274031 | — | IC50 | = | 15220.0 | nM | 4.82 |
| CHEMBL56146 | — | IC50 | = | 15150.0 | nM | 4.82 |
| CHEMBL291931 | — | IC50 | = | 17480.0 | nM | 4.76 |
| CHEMBL119224 | — | IC50 | = | 19080.0 | nM | 4.72 |
| CHEMBL325533 | — | IC50 | = | 22730.0 | nM | 4.64 |